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目的对甲巯咪唑水凝胶贴剂治疗甲状腺功能亢进症(甲亢)的药效学进行研究。方法通过灌服甲状腺片进行Wistar大鼠甲亢造模,药效学实验设甲巯咪唑水凝胶贴剂低、中、高剂量组,甲巯咪唑片剂组,甲亢阳性对照组和阴性对照组。给药后以大鼠血清中游离三碘甲腺原氨酸(FT3)、游离甲状腺素(FT4)、促甲状腺激素(TSH)值和肛温、平均日单位体重进食量为指标进行药效学评价。结果治疗4周后,甲巯咪唑水凝胶贴剂中剂量组、高剂量组和甲巯咪唑片剂组大鼠肛温、平均日单位体重进食量与甲亢阳性对照组比较有显著性差异(P<0.05或P<0.01);血清FT3、FT4、TSH指标均已处于正常范围,其中,血清FT4指标较甲亢阳性对照组有非常显著性差异(P<0.01)。结论甲巯咪唑水凝胶贴剂中、高剂量组对甲亢大鼠甲状腺激素的合成有较好的抑制作用。水凝胶贴剂有可能开发为治疗甲亢的甲巯咪唑新剂型。
Objective To study the pharmacodynamics of methimazole hydrogel patch in the treatment of hyperthyroidism (hyperthyroidism). Methods Thyroid gland was used to make hyperthyroidism model in Wistar rats. The pharmacodynamics experiments were divided into four groups: low, middle and high dosage of methimazole hydrogel patch, methimazole tablet, positive control group and negative control group . After administration, the pharmacodynamics of free triiodothyronine (FT3), free thyroxine (FT4), thyroid stimulating hormone (TSH), rectal temperature and mean body weight per daily intake Evaluation. Results After 4 weeks of treatment, the rectal temperature, mean daily body weight intake of rats in the middle dose group, high dose group and methimazole group of methimazole hydrogel patch were significantly different from those in the positive control group P <0.05 or P <0.01). Serum levels of FT3, FT4 and TSH were all in the normal range. Serum FT4 index was significantly different from that of HCC positive control group (P <0.01). Conclusions Methimazole hydrogel patch can effectively inhibit thyroid hormone synthesis in hyperthyroid rats. Hydrogel patches are likely to be developed as new methimazole dosage forms for the treatment of hyperthyroidism.